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In Vitro Evaluation of Serine Hydrolase Inhibitors

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Methods in Pharmacology and Toxicology

Part of the book series: Methods in Pharmacology and Toxicology

Abstract

Serine hydrolases are important in a variety of physiological processes and can be important pharmacological and toxicological molecular targets. A modified photometric method suitable for evaluating inhibition of the serine hydrolases acetylcholinesterase, butyrylcholinesterase, and monoacylglycerol lipase is described. The same reagents and protocol are used for each of the three different enzymes, with the only difference being the substrate. Kinetic considerations for reversible or irreversible inhibitors are discussed. This versatile assay can be used to quickly characterize inhibitory actions (IC50) of test compounds on the three hydrolases, with simple modifications allowing kinetic characterizations (Ki, k2, ki).

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Authors and Affiliations

  1. Center for Veterinary Health Sciences, Oklahoma State University, Stillwater, OK, USA

    Carey Pope & Kirstin Hester

  2. New Jersey Medical School, Rutgers University, Newark, NJ, USA

    Lester Sultatos

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  1. Carey Pope
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  2. Kirstin Hester
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  3. Lester Sultatos
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Correspondence to Carey Pope .

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Pope, C., Hester, K., Sultatos, L. (2018). In Vitro Evaluation of Serine Hydrolase Inhibitors. In: Methods in Pharmacology and Toxicology. Humana Press. https://doi.org/10.1007/7653_2018_11

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  • DOI: https://doi.org/10.1007/7653_2018_11

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